Zotepine is a potent antipsychotic and antidepressive drug, which was developed in Japan and used in many countries for the treatment of schizophrenia. Zotepine has high affinity to D2, 5-HT2A, 5-HT2C, 5-HT6, 5-HT7, alpha1A, H1, and D1 receptors at therapeutically relevant concentrations and has similar affinities to 5-HT1A, alpha2A, and M1 receptors at high concentrations. In human zotepine is metabolized to a major metabolite, norzotepine, which has profile similar to that of zotepine for important neurotransmitter receptors known to be responsible for zotepine antipsychotic activity.The drug is still available in Asia.

Talipexole is a D2 receptor agonist which was marketed in June 1996 in Japan for the treatment of Parkinson's disease. Clinical trials with talipexole in patients with Parkinson's disease demonstrated statistically significant improvements from baseline for parkinsonian symptoms including akinesia, rigidity, tremor and gait disturbances.

(+)-modafinil is an enantiomer of modafinil, a wake-promoting agent, that primarily affects areas of the brain involved in controlling wakefulness. (+)-enantiomer of modafinil was clarified to be S-configuration. The optical enantiomers of modafinil have similar pharmacological actions. Both modafinil enantiomers bind in vitro to the dopamine transporter and inhibit dopamine reuptake with the R- slightly more potent than the S-enantiomer. As a component of racemic mixture (+)-modafinil is indicated to improve wakefulness in adult patients with excessive sleepiness associated with narcolepsy, obstructive sleep apnea/hypopnea syndrome, and shift work sleep disorder.

Valerian is on the FDA’s list of substances that are generally recognised to be safe (GRAS). The root oil and extracts may be used as spice or seasoning. Valerian is most commonly used for sleep disorders. The essential oil of valerian contains a variety of compounds including valerenic acid and its derivatives, hydroxyvalerenic acid, acetoxyvalerenic acid and valerenal.

Raclopride is a salicylamide neuroleptic, that acts as a selective antagonist of D2 dopamine receptors both in vitro and in vivo. Tritium-labelled raclopride has properties that demonstrate its usefulness as a radioligand for the labelling of dopamine-D2 receptors : 3H-Raclopride has a high affinity for the rat and human dopamine-D2 receptors, the non-specific binding of 3H-raclopride is very low, not exceeding 5% of the total binding and the distribution of the 3H-raclopride binding sites in the brain closely correlates with the dopaminergic innervation. The binding of 3H-raclopride is blocked by dopamine-D2 agonists and antagonists, while the D1 agonist SKF 38393 and the Dl antagonist SCH 23390 have much less potency. The interaction of dopamine with 3H-raclopride binding results in a shallow competition curve, which suggests that 3H-raclopride, similar to other dopamine-D2 radioligands, labels both high and low agonist affinity states of the dopamine-D2 receptor. The in vivo receptor binding studies performed with 3H-raclopride also demonstrate its favorable properties as a dopamine-D2 receptor marker in vivo In contrast to some other compounds used as radioligands, raclopride enters the brain readily and binds with a low component of non-specific binding in all dopamine-rich brain areas. A saturation curve may be achieved in vivo binding studies since injections of increasing concentrations of 3H-raclopride appears to be saturated at concentrations above 25 mkCi (corresponding to approximately 5 nmol/kg). Raclopride antagonizes apomorphine-induced hyperactivity in the rat at low doses (ED50 = 130 nM/kg i.p.) but induces catalepsy only at much higher doses (ED50 = 27 mkM/kg i.p.). Radiolabelled raclopride has been used as a ligand for in vitro and in vivo autoradiography in rat and primate brains. Raclopride C 11 is used with positron emission tomography (PET) as a clinical research tool to determine dopamine type 2 (D 2) receptor density in the human brain under normal and pathological conditions. For example, raclopride C 11 used in PET studies has served to confirm the age-related decrease in striatal dopamine D2 receptor density, which may be associated with a decline in the motor as well as cognitive functions. In patients with Alzheimer's disease, raclopride C 11 may be used to examine neuroreceptor distribution and quantities, which may help in the analysis of degenerative alterations of neuron populations and neuroreceptor systems in patients with this disease. In Huntington's disease, in which degeneration of neostriatal interneurons occurs (postsynaptic to the dopaminergic input), specific binding of raclopride C 11 to D 2 receptors may serve as one of the parameters in predicting performance in cognitive tasks.

Oxypertine (Equipertine, Forit, Integrin, Lanturil, Lotawin, Opertil) is a neuroleptic drug and was originally introduced as a treatment for schizophrenia in the 1960s. Oxypertine is an indole derivative with general properties similar to those of the phenothiazine, chlorpromazine. It has been given by mouth in the treatment of various psychoses including schizophrenia, mania, and disturbed behaviour, and of severe anxiety. Like reserpine and tetrabenazine, oxypertine depletes catecholamines, though not serotonin, possibly underlying its neuroleptic efficacy. The molecular structure is strongly similar to solypertine and milipertine.

Chlorpromazine pamoate (also known as chlorpromazine embonate) is a salt of pamoic acid and a chlorpromazine. Pamoate salts are used in pharmaceutical formulations because they show slow dissolution and are useful in formulations where extended duration of action is required. Chlorpromazine is a phenothiazine antipsychotic. It also exerts sedative and antiemetic activity. The precise mechanism whereby the therapeutic effects of chlorpromazine are produced is not known. It has a wide range of activity arising from its depressant actions on the CNS and its alpha-adrenergic blocking and antimuscarinic activities. Chlorpromazine is a dopamine inhibitor; the turnover of dopamine in the brain is also increased. There is some evidence that the antagonism of central dopaminergic function, especially at the D2-dopaminergic receptor, is related to therapeutic effect in psychotic conditions.

Sulpiride is an atypical antipsychotic drug (although some texts have referred to it as a typical antipsychotic) of the benzamide class used mainly in the treatment of psychosis associated with schizophrenia and major depressive disorder, and sometimes used in low dosage to treat anxiety and mild depression. Sulpiride is commonly used in Europe, Russia and Japan. Sulpiride is a selective antagonist at dopamine D2 and D3 receptors. This action dominates in doses exceeding 600 mg daily. In doses of 600 to 1,600 mg sulpiride shows mild sedating and antipsychotic activity. Its antipsychotic potency compared to chlorpromazine is only 0.2 (1/5). In low doses (in particular 50 to 200 mg daily) its prominent feature is antagonism of presynaptic inhibitory dopamine receptors accounting for some antidepressant activity and a stimulating effect. Therefore, it is in these doses used as a second line antidepressant. Racemic and L-sulpiride significantly decreased stimulated serum gastrin concentration, but they did not affect fasting serum gastrin or basal and stimulated gastric acidity. D-sulpiride significantly decreased gastric acid secretion, without affecting serum gastrin levels.

Bromperidol (marketed as Bromidol, Bromodol) is a butyrophenone derivative. It is a potent and long-acting neuroleptic, used as an antipsychotic in the treatment of schizophrenia. It was discovered at Janssen Pharmaceutica in 1966. Bromperidol is a bromine analog of Haloperidol hydrochloride (sc-203593) which functions as a D2DR (dopamine D2 receptor) antagonist. Studies suggest that cytochrome CYP3A4 catalyzes the dehydration of Bromperidol and N-dealkylation of Bromperidol. In addition, CYP3A4 can oxidize N-dealkylated Bromperidol back into Bromperidol. Alternately, Bromperidol antagonizes the Neuroendocrine DA receptors which regulate hypothalamic LH-RH release.